Page last updated: 2024-11-12

famitinib

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Description

famitinib: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	16662431
CHEMBL ID	1278146
SCHEMBL ID	137251
MeSH ID	M0588957

Synonyms (30)

Synonym
(z)-2-(5-fluoro-2-oxo-1,2-dihydroindol-3-ylidenemethyl)-5-(2-diethylaminoethyl)-3-methyl-1,5,6,7-tetrahydropyrrolo-[3,2-c]pyridin-4-one
shr-1020
bdbm50331023
shr1020
CHEMBL1278146 ,
famitinib
unii-768fw21j3l
1044040-56-3
famitinib, (z)
5-(2-(diethylamino)ethyl0-2-9(z)-(5-fluoro-2-oxo-1h-indol-3-ylidene)methyl)-3-methyl-6,7-dihydro-1h-pyrrolo(3,2-c)pyridin-4(5h)-one
768fw21j3l ,
4h-pyrrolo(3,2-c)pyridin-4-one, 5-(2-(diethylamino)ethyl)-2-((z)-(5-fluoro-1,2-dihydro-2-oxo-3h-indol-3-ylidene)methyl)-1,5,6,7-tetrahydro-3-methyl-
famitinib [inn]
(z)-5-(2-(diethylamino)ethyl)-2-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-3-methyl-6,7-dihydro-1h-pyrrolo(3,2-c)pyridin-4(5h)-one
4h-pyrrolo(3,2-c)pyridin-4-one, 5-(2-(diethylamino)ethyl)-2-((5-fluoro-1,2-dihydro-2-oxo-3h-indol-3-ylidene)methyl)-1,5,6,7-tetrahydro-3-methyl-
famitinib [who-dd]
945380-27-8
shr 1020
compound 9 [pmid: 21028894]
5-(2-diethylaminoethyl)-2-[(z)-(5-fluoro-2-oxo-1h-indol-3-ylidene)methyl]-3-methyl-6,7-dihydro-1h-pyrrolo[4,5-c]pyridin-4-one
gtpl7886
SCHEMBL137251
DB11741
Q27077275
(z)-5-(2-(diethylamino)ethyl)-2-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-3-methyl-1,5,6,7-tetrahydro-4h-pyrrolo[3,2-c]pyridin-4-one
5-(2-(diethylamino)ethyl)-2-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-3-methyl-1,5,6,7-tetrahydro-4h-pyrrolo[3,2-c]pyridin-4-one
5-[2-(diethylamino)ethyl]-2-[(z)-(5-fluoro-2-oxo-1h-indol-3-ylidene)methyl]-3-methyl-6,7-dihydro-1h-pyrrolo[3,2-c]pyridin-4-one
MS-27081
EX-A6762
STARBLD0044024

Research Excerpts

Overview

Famitinib is a tyrosine kinase inhibitor targeting VEGFR2, PDGFR, and c-kit. It is under clinical investigation for the treatment of solid tumors.

Excerpt	Reference	Relevance
"Famitinib is a tyrosine kinase inhibitor targeting VEGFR2, PDGFR, and c-kit."	( Famitinib with Camrelizumab and Nab-Paclitaxel for Advanced Immunomodulatory Triple-Negative Breast Cancer (FUTURE-C-Plus): An Open-Label, Single-Arm, Phase II Trial. Cao, AY; Chai, WJ; Chen, CM; Chen, L; Chen, X; Di, GH; Fan, L; Guo, X; Hou, YF; Hu, X; Hu, Z; Huang, XY; Jiang, YZ; Li, JJ; Liu, GY; Ma, XY; Shao, ZM; Sun, XJ; Wang, ZH; Wu, J; Wu, SY; Xu, Y; Yang, WT; Yu, KD; Zhao, S; Zhu, XY; Zou, JJ, 2022)	2.89
"Famitinib is an oral, small-molecule, multi-targeted tyrosine kinase inhibitor under clinical investigation for the treatment of solid tumors. "	( The effect of rifampin on the pharmacokinetics of famitinib in healthy subjects. Cao, Y; Fu, Y; Gao, X; Jiang, X; Li, T; Li, X; Lin, P; Liu, Y; Shi, P; Sun, F; Wang, C; Zhang, Y, 2022)	2.42
"Famitinib is a tyrosine kinase inhibitor under clinical investigation for the treatment of solid tumors. "	( Effect of Dietary Intake on the Pharmacokinetics of the Multitargeted Receptor Tyrosine Kinase Inhibitor Famitinib: Results From a Phase 1 Study in Healthy Chinese Participants. Li, S; Rao, J; Shi, G; Wen, Q; Zhang, X; Zhao, H, 2023)	2.57
"Famitinib is a small-molecule multikinase inhibitor, with promising anticancer activities."	( Famitinib versus placebo in the treatment of refractory metastatic colorectal cancer: a multicenter, randomized, double-blinded, placebo-controlled, phase II clinical trial. Ba, Y; Bai, YX; Bi, JW; Ding, KF; Feng, JP; Lei, J; Li, J; Lin, LZ; Liu, YP; Ma, LW; Shen, L; Shi, CM; Wang, D; Wang, JW; Wang, KM; Wu, CP; Wu, G; Xiong, JP; Xu, RH; Yang, Q; Yu, H, 2017)	2.62
"Famitinib is a tyrosine kinase inhibitor against multiple targets, including vascular endothelial growth factor receptor 2/3, platelet-derived growth factor receptor, and stem cell factor receptor (c-kit). "	( Famitinib in combination with concurrent chemoradiotherapy in patients with locoregionally advanced nasopharyngeal carcinoma: a phase 1, open-label, dose-escalation Study. Cao, K; Chen, Q; Guo, L; Guo, S; Guo, X; Guo, Y; Han, F; He, Q; Li, Y; Liang, Y; Liu, H; Liu, L; Liu, N; Ma, J; Mai, H; Mo, H; Mo, Y; Sun, R; Sun, X; Tang, L; Tang, Q; Wang, J; Wang, P; Xie, C; Yang, X; Ye, Y; Zeng, M; Zhang, L, 2018)	3.37
"Famitinib is a novel and potent multitargeting receptor tyrosine kinase inhibitor. "	( Famitinib in metastatic renal cell carcinoma: a single center study. Chang, CX; Jiang, HY; Ma, JH; Qin, Q; Wang, JW; Zhang, W; Zhou, AP, 2013)	3.28
"Famitinib is an inhibitor of multiple tyrosine kinases mainly targeting VEGFR-2."	( Hypothyroidism as a potential biomarker of efficacy of famitinib, a novel VEGFR-2 inhibitor in metastatic breast cancer. Cao, J; Hu, X; Lv, F; Wang, B; Wang, L; Wang, Z; Zhang, J, 2014)	1.37
"Famitinib is a novel tyrosine kinase inhibitor. "	( Famitinib enhances nasopharyngeal cancer cell radiosensitivity by attenuating radiation-induced phosphorylation of platelet-derived growth factor receptor and c-kit and inhibiting microvessel formation. Huang, J; Ma, J; Mu, X; Qin, Y; Wu, G; Xu, S; Yang, K; Zhang, Z; Zhou, H, 2015)	3.3
"Famitinib is a novel multi-targeted receptor tyrosine kinase inhibitor under development for cancer treatment. "	( Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Chen, X; Diao, X; Gao, Z; Guo, Z; Jiang, H; Xie, C; Zhang, L; Zhong, D; Zhou, J, 2013)	2.12

Actions

Excerpt	Reference	Relevance
"Famitinib-related TSH increase may be an early indicator of its efficacy."	( Hypothyroidism as a potential biomarker of efficacy of famitinib, a novel VEGFR-2 inhibitor in metastatic breast cancer. Cao, J; Hu, X; Lv, F; Wang, B; Wang, L; Wang, Z; Zhang, J, 2014)	1.37

Toxicity

Excerpt	Reference	Relevance
" The most common ≥grade 3 treatment-related adverse events were hypertension (32."	( Antitumor activity and safety of camrelizumab plus famitinib in patients with platinum-resistant recurrent ovarian cancer: results from an open-label, multicenter phase 2 basket study. Gao, Y; Hu, W; Lou, G; Pan, M; Peng, J; Shi, H; Sun, R; Wang, L; Wang, Q; Wu, X; Xia, L; Zhang, Y; Zhou, Q; Zhou, X; Zhu, J, 2022)	0.97

Pharmacokinetics

This study is to establish physiologically based pharmacokinetic (PBPK) models of famitinib in rat and monkey. The aim is to predict the pharmacokinetics and tissue distribution of fam it in human based on the PBPK models.

Excerpt	Reference	Relevance
" The pharmacokinetic profile and various biomarkers were evaluated during the first cycle."	( Phase I study of the safety, pharmacokinetics and antitumor activity of famitinib. Chang, C; Chen, X; Jiang, H; Lou, D; Qin, Q; Wang, J; Zhang, W; Zhong, D; Zhou, A, 2013)	0.62
" Pharmacokinetic studies revealed no significant accumulation of famitinib or its major metabolite, M3."	( Phase I study of the safety, pharmacokinetics and antitumor activity of famitinib. Chang, C; Chen, X; Jiang, H; Lou, D; Qin, Q; Wang, J; Zhang, W; Zhong, D; Zhou, A, 2013)	0.86
"This study is to establish physiologically based pharmacokinetic (PBPK) models of famitinib in rat and monkey, and then to predict the pharmacokinetics and tissue distribution of famitinib in human based on the PBPK models."	( [Predicting pharmacokinetics of anti-cancer drug, famitinib in human using physiologically based pharmacokinetic model]. Chen, XY; Gao, ZW; Yu, MM; Zhong, DF, 2014)	0.88
" Pharmacokinetic parameters were calculated using noncompartmental analysis and safety was assessed."	( The effect of rifampin on the pharmacokinetics of famitinib in healthy subjects. Cao, Y; Fu, Y; Gao, X; Jiang, X; Li, T; Li, X; Lin, P; Liu, Y; Shi, P; Sun, F; Wang, C; Zhang, Y, 2022)	0.97
" Here, a 3-period crossover trial investigated the effect of high-fat or low-fat food intake on the single-dose pharmacokinetic properties of oral famitinib."	( Effect of Dietary Intake on the Pharmacokinetics of the Multitargeted Receptor Tyrosine Kinase Inhibitor Famitinib: Results From a Phase 1 Study in Healthy Chinese Participants. Li, S; Rao, J; Shi, G; Wen, Q; Zhang, X; Zhao, H, 2023)	1.32

Compound-Compound Interactions

HS-10296 and famitinib exhibit significant synergistic antitumor activity. Third-generation EGFR inhibitor combined with VEGFR inhibitor provides a promising strategy in the treatment of EGFR-mutant NSCLC.

Excerpt	Reference	Relevance
"Collectively, our results indicate that HS-10296 and famitinib exhibit significant synergistic antitumor activity, suggesting that the third-generation EGFR inhibitor combined with VEGFR inhibitor provides a promising strategy in the treatment of EGFR-mutant NSCLC."	( Third-generation EGFR inhibitor HS-10296 in combination with famitinib, a multi-targeted tyrosine kinase inhibitor, exerts synergistic antitumor effects through enhanced inhibition of downstream signaling in EGFR-mutant non-small cell lung cancer cells. Fu, H; Fu, L; Li, Y; Lou, L; Quan, H; Zhang, M, 2021)	1.11
"To evaluate the potential gastric pH-dependent drug-drug interaction (DDI), safety and tolerability of famitinib co-administered with omeprazole in healthy subjects."	( Phase I study to evaluate of the gastric pH-dependent drug interaction between famitinib and the proton pump inhibitor omeprazole in healthy subjects. Cai, M; Dou, T; Hu, L; Qian, W; Sun, Q; Tang, L; Wang, H, 2022)	1.16

Bioavailability

Oral famitinib bioavailability is not affected by food intake. Patients with cancer do not need to consider dietary status when using famit inib.

Excerpt	Reference	Relevance
"Famitinib is well absorbed and extensively metabolized in cancer patients."	( Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Chen, X; Diao, X; Gao, Z; Guo, Z; Jiang, H; Xie, C; Zhang, L; Zhong, D; Zhou, J, 2013)	2.12
" In conclusion, oral famitinib bioavailability is not affected by food intake, implying that patients with cancer do not need to consider dietary status when using famitinib."	( Effect of Dietary Intake on the Pharmacokinetics of the Multitargeted Receptor Tyrosine Kinase Inhibitor Famitinib: Results From a Phase 1 Study in Healthy Chinese Participants. Li, S; Rao, J; Shi, G; Wen, Q; Zhang, X; Zhao, H, 2023)	1.44

Dosage Studied

Excerpt	Relevance	Reference
" Blood samples were collected before dosing (0 hour) to 192 hours after dosing, and famitinib concentrations in plasma were determined with validated liquid chromatography-tandem mass spectrometry."	( Effect of Dietary Intake on the Pharmacokinetics of the Multitargeted Receptor Tyrosine Kinase Inhibitor Famitinib: Results From a Phase 1 Study in Healthy Chinese Participants. Li, S; Rao, J; Shi, G; Wen, Q; Zhang, X; Zhao, H, 2023)	1.35

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Platelet-derived growth factor receptor beta	Homo sapiens (human)	IC50 (µMol)	0.0040	0.0006	0.8007	8.5000	AID536881
Mast/stem cell growth factor receptor Kit	Homo sapiens (human)	IC50 (µMol)	0.0020	0.0007	0.4708	10.0000	AID536879
Vascular endothelial growth factor receptor 2	Homo sapiens (human)	IC50 (µMol)	0.0035	0.0000	0.4830	8.8000	AID536880; AID536882
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (150)

Process	via Protein(s)	Taxonomy
signal transduction	Platelet-derived growth factor receptor beta	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Platelet-derived growth factor receptor beta	Homo sapiens (human)
positive regulation of cell population proliferation	Platelet-derived growth factor receptor beta	Homo sapiens (human)
positive regulation of phospholipase C activity	Platelet-derived growth factor receptor beta	Homo sapiens (human)
positive regulation of smooth muscle cell migration	Platelet-derived growth factor receptor beta	Homo sapiens (human)
peptidyl-tyrosine phosphorylation	Platelet-derived growth factor receptor beta	Homo sapiens (human)
positive regulation of cell migration	Platelet-derived growth factor receptor beta	Homo sapiens (human)
positive regulation of phosphoprotein phosphatase activity	Platelet-derived growth factor receptor beta	Homo sapiens (human)
regulation of actin cytoskeleton organization	Platelet-derived growth factor receptor beta	Homo sapiens (human)
cell migration involved in vasculogenesis	Platelet-derived growth factor receptor beta	Homo sapiens (human)
platelet-derived growth factor receptor-beta signaling pathway	Platelet-derived growth factor receptor beta	Homo sapiens (human)
positive regulation of metanephric mesenchymal cell migration by platelet-derived growth factor receptor-beta signaling pathway	Platelet-derived growth factor receptor beta	Homo sapiens (human)
aorta morphogenesis	Platelet-derived growth factor receptor beta	Homo sapiens (human)
cellular response to platelet-derived growth factor stimulus	Platelet-derived growth factor receptor beta	Homo sapiens (human)
positive regulation of cell proliferation by VEGF-activated platelet derived growth factor receptor signaling pathway	Platelet-derived growth factor receptor beta	Homo sapiens (human)
positive regulation of MAP kinase activity	Platelet-derived growth factor receptor beta	Homo sapiens (human)
positive regulation of mitotic nuclear division	Platelet-derived growth factor receptor beta	Homo sapiens (human)
phosphatidylinositol metabolic process	Platelet-derived growth factor receptor beta	Homo sapiens (human)
protein autophosphorylation	Platelet-derived growth factor receptor beta	Homo sapiens (human)
platelet-derived growth factor receptor signaling pathway	Platelet-derived growth factor receptor beta	Homo sapiens (human)
positive regulation of smooth muscle cell proliferation	Platelet-derived growth factor receptor beta	Homo sapiens (human)
positive regulation of calcium-mediated signaling	Platelet-derived growth factor receptor beta	Homo sapiens (human)
positive regulation of chemotaxis	Platelet-derived growth factor receptor beta	Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	Platelet-derived growth factor receptor beta	Homo sapiens (human)
cardiac myofibril assembly	Platelet-derived growth factor receptor beta	Homo sapiens (human)
cell chemotaxis	Platelet-derived growth factor receptor beta	Homo sapiens (human)
cell migration involved in coronary angiogenesis	Platelet-derived growth factor receptor beta	Homo sapiens (human)
retina vasculature development in camera-type eye	Platelet-derived growth factor receptor beta	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Platelet-derived growth factor receptor beta	Homo sapiens (human)
smooth muscle cell chemotaxis	Platelet-derived growth factor receptor beta	Homo sapiens (human)
metanephric glomerular mesangial cell proliferation involved in metanephros development	Platelet-derived growth factor receptor beta	Homo sapiens (human)
metanephric glomerular capillary formation	Platelet-derived growth factor receptor beta	Homo sapiens (human)
positive regulation of calcium ion import	Platelet-derived growth factor receptor beta	Homo sapiens (human)
positive regulation of reactive oxygen species metabolic process	Platelet-derived growth factor receptor beta	Homo sapiens (human)
positive regulation of DNA biosynthetic process	Platelet-derived growth factor receptor beta	Homo sapiens (human)
positive regulation of kinase activity	Platelet-derived growth factor receptor beta	Homo sapiens (human)
angiogenesis	Platelet-derived growth factor receptor beta	Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathway	Platelet-derived growth factor receptor beta	Homo sapiens (human)
multicellular organism development	Platelet-derived growth factor receptor beta	Homo sapiens (human)
ovarian follicle development	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
myeloid progenitor cell differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
lymphoid progenitor cell differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
immature B cell differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
mast cell chemotaxis	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of dendritic cell cytokine production	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
glycosphingolipid metabolic process	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
inflammatory response	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
signal transduction	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
spermatogenesis	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
spermatid development	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
germ cell migration	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
regulation of cell shape	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
visual learning	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
male gonad development	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of phospholipase C activity	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
cytokine-mediated signaling pathway	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
stem cell population maintenance	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
lamellipodium assembly	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
actin cytoskeleton organization	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
hemopoiesis	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
T cell differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
erythrocyte differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
melanocyte differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of pseudopodium assembly	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of mast cell cytokine production	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
somatic stem cell population maintenance	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
embryonic hemopoiesis	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
ectopic germ cell programmed cell death	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
intracellular signal transduction	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
hematopoietic stem cell migration	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
megakaryocyte development	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
Fc receptor signaling pathway	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
Kit signaling pathway	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
erythropoietin-mediated signaling pathway	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
regulation of cell population proliferation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT protein	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
negative regulation of programmed cell death	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
mast cell degranulation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of MAPK cascade	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
pigmentation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
tongue development	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of Notch signaling pathway	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of receptor signaling pathway via JAK-STAT	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
response to cadmium ion	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
protein autophosphorylation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of long-term neuronal synaptic plasticity	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
digestive tract development	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
stem cell differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
epithelial cell proliferation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of sound	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of DNA-binding transcription factor activity	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
negative regulation of developmental process	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
cell chemotaxis	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
mast cell differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
mast cell proliferation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of mast cell proliferation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
melanocyte migration	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
melanocyte adhesion	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of pyloric antrum smooth muscle contraction	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
regulation of bile acid metabolic process	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of colon smooth muscle contraction	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of small intestine smooth muscle contraction	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of vascular associated smooth muscle cell differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
negative regulation of reproductive process	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of cell migration	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
positive regulation of MAP kinase activity	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
multicellular organism development	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
B cell differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
hematopoietic progenitor cell differentiation	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
branching involved in blood vessel morphogenesis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of macroautophagy	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of mitochondrial depolarization	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of mitochondrial fission	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
angiogenesis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
ovarian follicle development	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
vasculogenesis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of protein phosphorylation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of endothelial cell proliferation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
lymph vessel development	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
cell migration involved in sprouting angiogenesis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of mesenchymal cell proliferation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
epithelial cell maturation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
endocardium development	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
endothelium development	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathway	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of cell population proliferation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
regulation of cell shape	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
mesenchymal cell proliferation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of endothelial cell migration	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
negative regulation of gene expression	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
peptidyl-tyrosine phosphorylation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of cell migration	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of BMP signaling pathway	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
embryonic hemopoiesis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
cellular response to vascular endothelial growth factor stimulus	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
vascular endothelial growth factor receptor-2 signaling pathway	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
peptidyl-tyrosine autophosphorylation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
vascular endothelial growth factor signaling pathway	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
surfactant homeostasis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of MAPK cascade	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
negative regulation of neuron apoptotic process	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of blood vessel endothelial cell migration	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
cell fate commitment	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of angiogenesis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
protein autophosphorylation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
vascular endothelial growth factor receptor signaling pathway	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
lung alveolus development	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
post-embryonic camera-type eye morphogenesis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
epithelial cell proliferation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of positive chemotaxis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of nitric-oxide synthase biosynthetic process	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of focal adhesion assembly	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
calcium ion homeostasis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
blood vessel endothelial cell differentiation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
vascular wound healing	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
semaphorin-plexin signaling pathway	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
stem cell proliferation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of cell migration involved in sprouting angiogenesis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
regulation of hematopoietic progenitor cell differentiation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
regulation of bone development	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
cellular response to hydrogen sulfide	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
negative regulation of endothelial cell apoptotic process	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of stem cell proliferation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of endothelial cell chemotaxis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of vasculogenesis	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
regulation of MAPK cascade	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
multicellular organism development	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
cell migration	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
endothelial cell differentiation	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
positive regulation of kinase activity	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (27)

Process	via Protein(s)	Taxonomy
protein kinase activity	Platelet-derived growth factor receptor beta	Homo sapiens (human)
protein tyrosine kinase activity	Platelet-derived growth factor receptor beta	Homo sapiens (human)
platelet activating factor receptor activity	Platelet-derived growth factor receptor beta	Homo sapiens (human)
platelet-derived growth factor receptor activity	Platelet-derived growth factor receptor beta	Homo sapiens (human)
platelet-derived growth factor beta-receptor activity	Platelet-derived growth factor receptor beta	Homo sapiens (human)
signaling receptor binding	Platelet-derived growth factor receptor beta	Homo sapiens (human)
platelet-derived growth factor receptor binding	Platelet-derived growth factor receptor beta	Homo sapiens (human)
protein binding	Platelet-derived growth factor receptor beta	Homo sapiens (human)
ATP binding	Platelet-derived growth factor receptor beta	Homo sapiens (human)
enzyme binding	Platelet-derived growth factor receptor beta	Homo sapiens (human)
protein kinase binding	Platelet-derived growth factor receptor beta	Homo sapiens (human)
vascular endothelial growth factor binding	Platelet-derived growth factor receptor beta	Homo sapiens (human)
platelet-derived growth factor binding	Platelet-derived growth factor receptor beta	Homo sapiens (human)
protease binding	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
protein tyrosine kinase activity	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activity	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
stem cell factor receptor activity	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
protein binding	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
ATP binding	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
cytokine binding	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
SH2 domain binding	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
protein homodimerization activity	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
metal ion binding	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
growth factor binding	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
protein tyrosine kinase activity	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activity	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
vascular endothelial growth factor receptor activity	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
integrin binding	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
protein binding	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
ATP binding	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
coreceptor activity	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
growth factor binding	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
vascular endothelial growth factor binding	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
identical protein binding	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
cadherin binding	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
Hsp90 protein binding	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Process	via Protein(s)	Taxonomy
nucleus	Platelet-derived growth factor receptor beta	Homo sapiens (human)
cytoplasm	Platelet-derived growth factor receptor beta	Homo sapiens (human)
Golgi apparatus	Platelet-derived growth factor receptor beta	Homo sapiens (human)
plasma membrane	Platelet-derived growth factor receptor beta	Homo sapiens (human)
focal adhesion	Platelet-derived growth factor receptor beta	Homo sapiens (human)
membrane	Platelet-derived growth factor receptor beta	Homo sapiens (human)
apical plasma membrane	Platelet-derived growth factor receptor beta	Homo sapiens (human)
cytoplasmic vesicle	Platelet-derived growth factor receptor beta	Homo sapiens (human)
lysosomal lumen	Platelet-derived growth factor receptor beta	Homo sapiens (human)
intracellular membrane-bounded organelle	Platelet-derived growth factor receptor beta	Homo sapiens (human)
plasma membrane	Platelet-derived growth factor receptor beta	Homo sapiens (human)
receptor complex	Platelet-derived growth factor receptor beta	Homo sapiens (human)
fibrillar center	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
acrosomal vesicle	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
extracellular space	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
plasma membrane	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
cell-cell junction	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
external side of plasma membrane	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
cytoplasmic side of plasma membrane	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
plasma membrane	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
receptor complex	Mast/stem cell growth factor receptor Kit	Homo sapiens (human)
extracellular region	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
nucleus	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
endosome	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
early endosome	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
endoplasmic reticulum	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
Golgi apparatus	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
plasma membrane	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
external side of plasma membrane	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
cell junction	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
membrane raft	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
anchoring junction	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
sorting endosome	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
plasma membrane	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
receptor complex	Vascular endothelial growth factor receptor 2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (17)

Assay ID	Title	Year	Journal	Article
AID536882	Inhibition of VEGFR2-induced cell proliferation in HUVEC after 72 hrs by sulforhodamine B method	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
AID536884	AUC in Sprague-Dawley rat at 40 mg/kg, po	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
AID536890	Antitumor activity against human HT-29 cells xenografted in BALB/cA nude mouse assessed as inhibition of tumor growth at 10 mg/kg, po administered 11 days after tumor implantation qd for 14 days	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
AID536885	Half life in Sprague-Dawley rat at 10 mg/kg, po and 10 mg/kg iv	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
AID536881	Inhibition of human PDGFRbeta after 30 mins by ELISA	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
AID536892	Toxicity in human HT-29 cells xenografted BALB/cA nude mouse assessed as weight loss at up to 30 mg/kg, po administered 11 days after tumor implantation qd for 14 days	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
AID536883	Cmax in Sprague-Dawley rat at 10 mg/kg, po and 10 mg/kg iv	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
AID536887	Volume of distribution in Sprague-Dawley rat at 10 mg/kg, po and 10 mg/kg iv	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
AID536880	Inhibition of human VEGFR2 after 30 mins by ELISA	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
AID536893	Toxicity in human HT-29 cells xenografted BALB/cA nude mouse assessed as mortality at up to 30 mg/kg, po administered 11 days after tumor implantation qd for 14 days	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
AID536879	Inhibition of c-Kit after 30 mins by ELISA	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
AID536889	Antitumor activity against human HT-29 cells xenografted in po dosed BALB/cA nude mouse assessed as inhibition of tumor growth administered 11 days after tumor implantation qd for 14 days	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
AID536888	Oral bioavailability in Sprague-Dawley rat at 10 mg/kg	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
AID536886	Clearance in Sprague-Dawley rat at 10 mg/kg, po and 10 mg/kg iv	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
AID1345506	Human kinase insert domain receptor (Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family)	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
AID1345590	Human platelet derived growth factor receptor beta (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family)	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
AID1345555	Human KIT proto-oncogene receptor tyrosine kinase (Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family)	2010	Journal of medicinal chemistry, Nov-25, Volume: 53, Issue:22	Novel potent orally active multitargeted receptor tyrosine kinase inhibitors: synthesis, structure-activity relationships, and antitumor activities of 2-indolinone derivatives.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (24)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	0 (0.00)	29.6817
2010's	12 (50.00)	24.3611
2020's	12 (50.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 29.50

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

Metric	This Compound (vs All)
Research Demand Index	29.50 (24.57)
Research Supply Index	3.56 (2.92)
Research Growth Index	5.87 (4.65)
Search Engine Demand Index	34.37 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (29.50)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	10 (41.67%)	5.53%
Reviews	1 (4.17%)	6.00%
Case Studies	1 (4.17%)	4.05%
Observational	0 (0.00%)	0.25%
Other	12 (50.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
omeprazole Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.. omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.. 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5.	8.8	1	1	aromatic ether; benzimidazoles; pyridines; sulfoxide
pyrroles 1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.	10.97	19	7	pyrrole; secondary amine
quinazolines Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.	3.23	1	0	azaarene; mancude organic heterobicyclic parent; ortho-fused heteroarene; quinazolines
platinum Platinum: A heavy, soft, whitish metal, resembling tin, with atomic number 78, atomic weight 195.084, symbol Pt. It is used in manufacturing equipment for laboratory and industrial use. It occurs as a black powder (platinum black) and as a spongy substance (spongy platinum) and may have been known in Pliny's time as alutiae.	9.72	1	1	elemental platinum; nickel group element atom; platinum group metal atom
paclitaxel Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).	8.74	2	0	taxane diterpenoid; tetracyclic diterpenoid	antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent
benzofurans Benzofurans: Compounds that contain a BENZENE ring fused to a furan ring.	3.23	1	0
su 11248 [no description available]	2.49	2	0	monocarboxylic acid amide; pyrroles	angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; immunomodulator; neuroprotective agent; vascular endothelial growth factor receptor antagonist
everolimus [no description available]	2.13	1	0	cyclic acetal; cyclic ketone; ether; macrolide lactam; primary alcohol; secondary alcohol	anticoronaviral agent; antineoplastic agent; geroprotector; immunosuppressive agent; mTOR inhibitor
icotinib [no description available]	3.23	1	0
ast 1306 AST 1306: an antineoplastic agent that inhibits epidermal growth factor receptors 1 and 2; structure in first source	3.23	1	0	quinazolines
hmpl-013 HMPL-013: a VEGF receptor antagonist; structure in first source	3.23	1	0
rifampin Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160)	8.33	1	0	cyclic ketal; hydrazone; N-iminopiperazine; N-methylpiperazine; rifamycins; semisynthetic derivative; zwitterion	angiogenesis inhibitor; antiamoebic agent; antineoplastic agent; antitubercular agent; DNA synthesis inhibitor; EC 2.7.7.6 (RNA polymerase) inhibitor; Escherichia coli metabolite; geroprotector; leprostatic drug; neuroprotective agent; pregnane X receptor agonist; protein synthesis inhibitor

Condition	Indicated	Relationship Strength	Studies	Trials
Epithelial Ovarian Cancer [description not available]	0	4.72	1	1
Carcinoma, Ovarian Epithelial A malignant neoplasm that originates in cells on the surface EPITHELIUM of the ovary and is the most common form of ovarian cancer. There are five histologic subtypes: papillary serous, endometrioid, mucinous, clear cell, and transitional cell. Mutations in BRCA1, OPCML, PRKN, PIK3CA, AKT1, CTNNB1, RRAS2, and CDH1 genes are associated with this cancer.	0	4.72	1	1
ER-Negative PR-Negative HER2-Negative Breast Cancer [description not available]	0	3.74	2	0
Triple Negative Breast Neoplasms Breast neoplasms that do not express ESTROGEN RECEPTORS; PROGESTERONE RECEPTORS; and do not overexpress the NEU RECEPTOR/HER-2 PROTO-ONCOGENE PROTEIN.	1	5.74	2	0
Bladder Cancer [description not available]	0	4.72	1	1
Urinary Bladder Neoplasms Tumors or cancer of the URINARY BLADDER.	0	4.72	1	1
Carcinoma, Transitional Cell A malignant neoplasm derived from TRANSITIONAL EPITHELIAL CELLS, occurring chiefly in the URINARY BLADDER; URETERS; or RENAL PELVIS.	0	4.72	1	1
Cancer of Lung [description not available]	0	2.76	2	0
Lung Neoplasms Tumors or cancer of the LUNG.	1	4.76	2	0
Thyroid Cancer, Anaplastic [description not available]	0	3.99	1	1
Cancer of the Thyroid [description not available]	0	3.99	1	1
Thyroid Neoplasms Tumors or cancer of the THYROID GLAND.	0	3.99	1	1
Thyroid Carcinoma, Anaplastic An aggressive THYROID GLAND malignancy which generally occurs in IODINE-deficient areas in people with previous thyroid pathology such as GOITER. It is associated with CELL DEDIFFERENTIATION of THYROID CARCINOMA (e.g., FOLLICULAR THYROID CARCINOMA; PAPILLARY THYROID CANCER). Typical initial presentation is a rapidly growing neck mass which upon metastasis is associated with DYSPHAGIA; NECK PAIN; bone pain; DYSPNEA; and NEUROLOGIC DEFICITS.	0	3.99	1	1
Benign Neoplasms [description not available]	0	4.77	3	2
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	1	7.95	6	4
Carcinoma, Non-Small Cell Lung [description not available]	0	2.31	1	0
Carcinoma, Non-Small-Cell Lung A heterogeneous aggregate of at least three distinct histological types of lung cancer, including SQUAMOUS CELL CARCINOMA; ADENOCARCINOMA; and LARGE CELL CARCINOMA. They are dealt with collectively because of their shared treatment strategy.	1	4.31	1	0
Adenocarcinoma Of Kidney [description not available]	0	5.01	4	2
Cancer of Kidney [description not available]	0	5.01	4	2
Carcinoma, Renal Cell A heterogeneous group of sporadic or hereditary carcinoma derived from cells of the KIDNEYS. There are several subtypes including the clear cells, the papillary, the chromophobe, the collecting duct, the spindle cells (sarcomatoid), or mixed cell-type carcinoma.	1	7.01	4	2
Kidney Neoplasms Tumors or cancers of the KIDNEY.	0	5.01	4	2
Metastase [description not available]	0	5.86	2	2
Colorectal Cancer [description not available]	0	9.45	1	1
Neoplasm Metastasis The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.	0	5.86	2	2
Colorectal Neoplasms Tumors or cancer of the COLON or the RECTUM or both. Risk factors for colorectal cancer include chronic ULCERATIVE COLITIS; FAMILIAL POLYPOSIS COLI; exposure to ASBESTOS; and irradiation of the CERVIX UTERI.	1	6.45	1	1
Nasopharyngeal Carcinoma A carcinoma that originates in the EPITHELIUM of the NASOPHARYNX and includes four subtypes: keratinizing squamous cell, non-keratinizing, basaloid squamous cell, and PAPILLARY ADENOCARCINOMA. It is most prevalent in Southeast Asian populations and is associated with EPSTEIN-BARR VIRUS INFECTIONS. Somatic mutations associated with this cancer have been identified in NPCR, BAP1, UBAP1, ERBB2, ERBB3, MLL2, PIK3CA, KRAS, NRAS, and ARID1A genes.	0	8.93	2	1
Blood Pressure, High [description not available]	0	3.47	1	1
Sarcoma, Epithelioid [description not available]	0	3.47	1	1
Hypertension Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.	0	3.47	1	1
Sarcoma A connective tissue neoplasm formed by proliferation of mesodermal cells; it is usually highly malignant.	0	3.47	1	1
Breast Cancer [description not available]	0	9.4	1	1
Central Hypothyroidism [description not available]	0	4.4	1	1
Breast Neoplasms Tumors or cancer of the human BREAST.	1	7.83	2	2
Hypothyroidism A syndrome that results from abnormally low secretion of THYROID HORMONES from the THYROID GLAND, leading to a decrease in BASAL METABOLIC RATE. In its most severe form, there is accumulation of MUCOPOLYSACCHARIDES in the SKIN and EDEMA, known as MYXEDEMA. It may be primary or secondary due to other pituitary disease, or hypothalamic dysfunction.	0	9.4	1	1
Carcinoma, Anaplastic [description not available]	0	2.11	1	0
Cancer of Nasopharynx [description not available]	0	2.11	1	0
Angiogenesis, Pathologic [description not available]	0	2.52	2	0
Carcinoma A malignant neoplasm made up of epithelial cells tending to infiltrate the surrounding tissues and give rise to metastases. It is a histological type of neoplasm and not a synonym for cancer.	0	2.11	1	0
Nasopharyngeal Neoplasms Tumors or cancer of the NASOPHARYNX.	1	4.11	1	0
Neuroendocrine Tumors Tumors whose cells possess secretory granules and originate from the neuroectoderm, i.e., the cells of the ectoblast or epiblast that program the neuroendocrine system. Common properties across most neuroendocrine tumors include ectopic hormone production (often via APUD CELLS), the presence of tumor-associated antigens, and isozyme composition.	0	2.13	1	0

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